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Table 2 Other MKIs for MAPK are being tested for different types of thyroid cancer but at the time of writing this article, none have reached phase III trials

From: Novel targeted therapies and immunotherapy for advanced thyroid cancers

Drug Drug targets Phase Dosage Patients Partial response RR (%) Progression-free survival PFS (months) Adverse effects (%) Drug discontinuation
Multikinase inhibitors
Axitinib [130] VEGFR, PDGFR, c-kit II starting dose of 5 mg twice daily 60 30 18.1 Fatigue (50%), diarrhea (48%), nausea (33%), anorexia (30%), hypertension (28%), stomatitis (25%), weight loss (25%), and headache (22%) 32 patients, 8 of them due to treatment side effects
Motesanib [131] VEGFR, PDGFR, c-kit II 125 mg/day orally for up to 48 weeks 93 14 9.3 Diarrhea (59%), hypertension (56%), fatigue (46%), and weight loss (40%) 61 patients, 12 of them due to treatment side effects
Sunitinib [132] PDGFR, FLT3, c-kit, VEGFR, RET II 37.5 mg/day orally 35 31 12.8 Neutropenia (34%), fatigue (11%), HFS (17%), diarrhea (17%), and leukopenia (31%) 4 patients due to treatment side effects
Pazopanib [133] VEGFR, PDGFR, c-kit II 800 mg/day orally in 4-week cycle 37 49 11.7 Fatigue (78%), skin and hair hypopigmentation (75%), diarrhea (73%), and nausea (73%) 27 patients, 2 of them due to treatment side effects
Dovitinib [134] FGFR, and (VEGFR) II 500 mg/day orally for five consecutive days, followed by a 2-day rest every week. 40 20.5 5.4 Diarrhea (54%), anorexia (36%), vomiting (26%), fatigue (23%), and nausea (21%) 12 patients
Imatinib [135] BCR-ABL, PDGFR-α, PDGFR-β, c-fms, c-Kit, and RET II 600 mg/day orally 15 0 NR Hypothyroidism (60%), rash, malaise, and laryngeal mucosal swelling (13%) 10 patients, 3 of them due to treatment side effects
Selumetinib (AZD6244) [43] MEK-1/2 (one of MAPK), RAS, V600E BRAF II 100 mg twice daily for 28-days cycles 39 3 8 Rash (77%), fatigue (49%), diarrhea (49%), and peripheral edema (36%) Only 6 patients due to treatment side effects
Selective BRAF inhibitors
Dabrafenib [136] BRAF I 150 mg twice daily or 100 mg three times daily 14 29 11.3 skin papillomas (57%), hyperkeratosis (36%), alopecia (29%), elevated lipase (7%), grade 3 elevated amylase (7%), grade 3 fatigue (7%), grade 3 febrile neutropenia (7%), and grade 3 cutaneous squamous cell carcinoma (7%) None
Vemurafenib [137] BRAF II 960 mg orally twice daily 51 35 15.6 squamous cell carcinoma of the skin (23.5%), lymphopenia (8%), and increased γ-glutamyl-transferase (8%)